Design, synthesis and cytotoxicity studies of novel pyrazolo[1, 5-a]pyridine derivatives

• Published in: European journal of medicinal chemistry Vol. 126; pp. 277 - 285
• Main Authors: Ravi, Chitrakar, Qayum, Arem, Chandra Mohan, Darapaneni, Singh, Shashank K., Adimurthy, Subbarayappa
• Format: Journal Article
• Language: English
• Published: PARIS Elsevier Masson SAS 27.01.2017; Elsevier
• Subjects: Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Apoptosis - drug effects; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry Techniques, Synthetic; Chemistry, Medicinal; Cytotoxicity; Dose-Response Relationship, Drug; Drug Design; Growth inhibition; Humans; Life Sciences & Biomedicine; MCF-7 cells; Pharmacology & Pharmacy; Pyrazoles - chemistry; Pyrazolo[1, 5–a]pyridines; Pyridines - chemical synthesis; Pyridines - chemistry; Pyridines - pharmacology; Science & Technology; SRB assay; Cytotoxicity; Growth inhibition; MCF-7 cells; Pyrazolo[1, 5–a]pyridines; SRB assay; AZAINDOLE DERIVATIVES; MCF-7 cells; RECEPTOR; CELL-CYCLE; Pyrazolo[1,5-a]pyridines; CANCER
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2016.11.037

Copper–mediated synthesis of various pyrazolo[1, 5–a]pyridine-3-carboxylates has been described. The biological activities of these molecules have been evaluated against various human cancer cell lines A549 (Lung adenocarcinoma cell line), MCF-7 (Breast carcinoma cell line), HCT-116 (Colon cancer cell line), and PC-3 (Prostate cancer cell line) through SRB assay. Compound 247 led to accumulation MCF-7 cells in G1-phase and revealed its important role in mitotic cell cycle progression. Against various cancer cell lines (A549, PC-3, HCT-116, MCF-7) determined by SRB assay. [Display omitted] •This work highlights the synthesis of substituted pyrazolo[1,5-a]pyridine derivatives as anticancer agents.•In vitro screening of target pyrazolo[1, 5-a]pyridines against various human cancer cell lines.•Determination of IC50 against various human cancer cell lines.•Pyrazolo[1, 5-a]pyridines are active anticancer, antimicrobial, antiviral, antipsychotic, etc.